Antihistamines for Systemic Use

Antihistamines for Systemic Use
Accession Number
Not Available
ATC Classification
DrugDrug Description
ClemastineAn antihistamine with sedative and anticholinergic effects used to treat the symptoms of allergic rhinitis.
CetirizineA selective Histamine-1 antagonist drug used in allergic rhinitis and chronic urticaria.
TerfenadineFor the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
BuclizineFor prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems).
DoxylamineAn antihistamine used to treat insomnia and allergy symptoms and is used with pyridoxine in the treatment of nausea and vomiting in pregnancy.
ThiethylperazineFor the treatment or relief of nausea and vomiting.
DexbrompheniramineAn antihistamine used to treat allergy symptoms including upper respiratory tract symptoms.
TriprolidineA sedating antihistamine combined with pseudoephedrine and guaifenesin in various types of cold and allergy medications to relieve allergy symptoms, hay fever and common cold symptoms, and to aid in sleep.
CyproheptadineA combined serotonin and histamine antagonist used in the treatment of allergic symptoms, for appetite stimulation, and off-label in the treatment of serotonin syndrome.
LoratadineA second generation antihistamine used to manage the symptoms of allergic rhinitis.
AstemizoleA second generation antihistamine used to treat allergy symptoms.
TrimethobenzamideAn antiemetic used to treat postoperative nausea and vomiting and nausea associated with gastroenteritis.
AzatadineAn H1 receptor antagonist used to treat perennial and allergic rhinitis as well as eustachian tube congestion.
MeclizineA histamine H1 antagonist used to treat nausea, vomiting, and dizziness associated with motion sickness.
CarbinoxamineA first generation antihistamine used to treat allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis, allergic reactions, and mild allergic reactions.
BrompheniramineA histamine H1 antagonist used to treat coughs, upper respiratory symptoms, and nasal congestion associated with allergies and the common cold.
MethdilazineUsed for the symptomatic relief of hypersensitivity reactions and particularly for the control of pruritic skin disorders
KetotifenA histamine H1 receptor blocker and mast cell stabilizer used to treat mild atopic asthma and allergic conjunctivitis.
FexofenadineA selective H1-antagonist for the symptomatic treatment of seasonal allergic rhinitis and chronic idiopathic urticaria.
DesloratadineA second generation tricyclic antihistamine used to treat seasonal and non seasonal allergic rhinitis, pruritus, and urticaria.
AzelastineA histamine H1-receptor antagonist used intranasally to treat allergic and vasomotor rhinitis and in an ophthalmic solution to treat allergic conjunctivitis.
PromethazineA first-generation antihistamine used for the treatment of allergic conditions, nausea and vomiting, and motion sickness.
MequitazineFor the treatment of Hay fever, urticaria (hives) and allergic rhinitis
DiphenhydramineA H1 receptor antihistamine used in the treatment of seasonal allergies, and various allergic reactions including sneezing, runny nose, itchy/watery eyes, itching of nose or throat, pruritus, urticaria, insect bites/stings, and allergic rashes.
ChlorpheniramineA histamine-H1 receptor antagonist indicated for the management of symptoms associated with upper respiratory allergies.
DiphenylpyralineAn antihistamine used for the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
CyclizineAn antihistamine and antiemetic drug used for the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo.
BromodiphenhydramineFor management of symptoms related to hay fever and other types of allergy and used to help bring up phlegm, thin secretions, and make a cough productive.
AlimemazineAn antihistamine agent used to prevent and relieve allergic conditions which cause pruritus and other allergic skin conditions, including urticaria.
PhenindamineUsed to treat sneezing, runny nose, itching, watery eyes, hives, rashes, itching, and other symptoms of allergies and the common cold.
MethapyrileneMethapyrilene, formerly marketed in many drug products, was shown to be a potent carcinogen. Manufacturers voluntarily withdrew methapyriline drug products from the market in May and June 1979.
ThenalidineWithdrawn from the Canadian, US, and UK markets in 1963 due to concerns involving neutropenia.
LevocetirizineAn H1-receptor antagonist used to treat symptoms associated with chronic allergic rhinitis and uncomplicated cases of chronic idiopathic urticaria.
AntazolineAn antihistamine agent used for the symptomatic treatment of nasal congestion and allergic conjunctivitis.
ChloropyramineFor the treatment of allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) conditions.
IsothipendylFor the topical treatment of itching associated with allergic reactions.
ChlorcyclizineChlorcyclizine is a first generation phenylpiperazine class antihistamine used to treat urticaria, rhinitis, pruritus, and other allergy symptoms. Chlorcyclizine also has some local anesthetic, anticholinergic, and antiserotonergic properties, and can...
AcrivastineAn antihistamine agent used for the symptomatic relief of seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion.
ThonzylamineThozylamine is indicated for use in the symptomatic control of allergic rhinitis or other upper respiratory allergic symptoms [FDA Label]. It is typically a part of combination over the counter...
BilastineA peripheral histamine H1-antagonist used to treat seasonal allergic rhinitis and chronic spontaneous urticaria.
RupatadineA selective histamine H1 receptor antagonist and platelet activating factor (PAF) antagonist used to treat allergic rhinitis.
EbastineEbastine is under investigation for the treatment of Irritable Bowel Syndrome (IBS). Ebastine has been investigated for the treatment of Urticaria.
MizolastineMizolastine is under investigation in clinical trial NCT01928316 (A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers).
OxatomideOxatomide has been used in trials studying the treatment of Muscular Dystrophy, Duchenne.
PimethixenePimethixene is approved for use in Brazil and is marketed under the trade name Muricalm. It is an anticholinergic used in the treatment of bronchitis.
TalastineNot Annotated
ThiazinamNot Annotated
DeptropineNot Annotated
HistapyrrodineNot Annotated
BamipineNot Annotated
SequifenadineNot Annotated
DexchlorpheniramineDexchlorpheniramine is a potent S-enantiomer of chlorpheniramine. The salt form dexchlorpheniramine maleate as the active ingredient is available as a prescription drug indicated for adjunctive therapy for allergic and anaphylactic...
TritoqualineNot Annotated
QuifenadineNot Annotated
MebhydrolinNot Annotated
OxomemazineNot Annotated
HydroxyethylpromethazineNot Annotated
PyrrobutamineNot Annotated
TripelennamineA histamine H1 antagonist used to treat hypersensitivity reactions, coughs, and the common cold.
PheniramineAn antihistamine used to treat allergic rhinitis and pruritus.
MepyramineAn antihistamine agent used for the symptomatic treatment of allergy, hypersensitivity reactions, and pruritic skin disorders.
DimetindeneIndicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hey fever and perennial rhinitis, food and drug allergies; pruritus of various origins, except...
ChlorphenoxamineChlorphenoxamine is marketed under the name Phenoxene. It is an antihistamine and anticholinergic used to treat itching as well as for its antiparkinsonian effect.
Drugs & Drug Targets
ClemastineHistamine H1 receptortarget
ClemastineCytochrome P450 2D6enzyme
CetirizineHistamine H1 receptortarget
CetirizineP-glycoprotein 1transporter
TerfenadineHistamine H1 receptortarget
TerfenadinePotassium voltage-gated channel subfamily H member 2target
TerfenadineCytochrome P450 3A4enzyme
TerfenadineCytochrome P450 2D6enzyme
TerfenadineMuscarinic acetylcholine receptor M3target
TerfenadineCytochrome P450 3A5enzyme
TerfenadineCytochrome P450 3A7enzyme
TerfenadineP-glycoprotein 1transporter
TerfenadineCytochrome P450 2C8enzyme
TerfenadineCytochrome P450 2J2enzyme
TerfenadineMuscarinic acetylcholine receptor M1target
TerfenadineMuscarinic acetylcholine receptor M5target
TerfenadineMuscarinic acetylcholine receptor M4target
TerfenadineMuscarinic acetylcholine receptor M2target
TerfenadineBile salt export pumptransporter
BuclizineHistamine H1 receptortarget
BuclizineMuscarinic acetylcholine receptor M1target
DoxylamineHistamine H1 receptortarget
DoxylamineMuscarinic acetylcholine receptortarget
DoxylamineCYP2B proteinenzyme
DoxylamineNuclear receptor subfamily 1 group I member 3target
ThiethylperazineDopamine D2 receptortarget
DexbrompheniramineHistamine H1 receptortarget
TriprolidineHistamine H1 receptortarget
Cyproheptadine5-hydroxytryptamine receptor 2Atarget
CyproheptadineHistamine H1 receptortarget
CyproheptadineMuscarinic acetylcholine receptor M1target
CyproheptadineMuscarinic acetylcholine receptor M2target
CyproheptadineMuscarinic acetylcholine receptor M3target
Cyproheptadine5-hydroxytryptamine receptor 2Ctarget
CyproheptadineUDP-glucuronosyltransferase 1-3enzyme
Cyproheptadine5-hydroxytryptamine receptor 7target
CyproheptadineUDP-glucuronosyltransferase 2B10enzyme
CyproheptadineUDP-glucuronosyltransferase 1-4enzyme
Cyproheptadine5-hydroxytryptamine receptor 2Btarget
CyproheptadineHistamine H2 receptortarget
CyproheptadineSolute carrier family 22 member 1transporter
CyproheptadineSerum albumincarrier
LoratadineHistamine H1 receptortarget
LoratadineCytochrome P450 3A4enzyme
LoratadineCytochrome P450 2C19enzyme
LoratadineCytochrome P450 2D6enzyme
LoratadineCytochrome P450 2C8enzyme
LoratadineP-glycoprotein 1transporter
LoratadinePotassium voltage-gated channel subfamily H member 2target
LoratadineBile salt export pumptransporter
LoratadineCytochrome P450 1A1enzyme
LoratadineCytochrome P450 1A2enzyme
LoratadineCytochrome P450 2B6enzyme
LoratadineCytochrome P450 2C9enzyme
LoratadineCytochrome P450 3A5enzyme
LoratadineUDP-glucuronosyltransferase 2B10enzyme
LoratadineUDP-glucuronosyltransferase 1-1enzyme
LoratadineUDP-glucuronosyltransferase 1-3enzyme
LoratadineUDP-glucuronosyltransferase 2B15enzyme
AstemizoleHistamine H1 receptortarget
AstemizolePotassium voltage-gated channel subfamily H member 2target
AstemizoleCytochrome P450 3A4enzyme
AstemizoleCytochrome P450 3A5enzyme
AstemizoleCytochrome P450 3A7enzyme
AstemizoleP-glycoprotein 1transporter
AstemizoleCytochrome P450 2D6enzyme
AstemizoleCytochrome P450 2J2enzyme
AstemizolePotassium voltage-gated channel subfamily H member 1target
AstemizoleMicrotubule-associated protein tautarget
AstemizoleBile salt export pumptransporter
AzatadineHistamine H1 receptortarget
AzatadineCytochrome P450 3A4enzyme
MeclizineHistamine H1 receptortarget
MeclizineNuclear receptor subfamily 1 group I member 3target
MeclizineCytochrome P450 2D6enzyme
MeclizineSerum albumincarrier
CarbinoxamineHistamine H1 receptortarget
BrompheniramineHistamine H1 receptortarget
BrompheniramineMuscarinic acetylcholine receptor M1target
BrompheniramineMuscarinic acetylcholine receptor M2target
BrompheniramineMuscarinic acetylcholine receptor M3target
BrompheniramineMuscarinic acetylcholine receptor M4target
BrompheniramineMuscarinic acetylcholine receptor M5target
MethdilazineHistamine H1 receptortarget
KetotifenHistamine H1 receptortarget
Ketotifen6-phosphogluconate dehydrogenase, decarboxylatingtarget
KetotifenUDP-glucuronosyltransferase 1-3enzyme
KetotifenUDP-glucuronosyltransferase 1-4enzyme
KetotifenUDP-glucuronosyltransferase 2B10enzyme
FexofenadineHistamine H1 receptortarget
FexofenadineP-glycoprotein 1transporter
FexofenadineSolute carrier organic anion transporter family member 2B1transporter
FexofenadineSolute carrier organic anion transporter family member 1A2transporter
FexofenadineSolute carrier organic anion transporter family member 1B1transporter
FexofenadineSolute carrier organic anion transporter family member 1B3transporter
FexofenadineSolute carrier family 22 member 8transporter
FexofenadineCanalicular multispecific organic anion transporter 1transporter
FexofenadineCanalicular multispecific organic anion transporter 2transporter
FexofenadineSerum albumincarrier
Fexofenadinealpha1-acid glycoproteincarrier
DesloratadineHistamine H1 receptortarget
DesloratadineP-glycoprotein 1transporter
AzelastineHistamine H1 receptortarget
AzelastineCytochrome P450 1A2enzyme
AzelastineCytochrome P450 2D6enzyme
AzelastineCytochrome P450 3A4enzyme
AzelastineCytochrome P450 2C19enzyme
AzelastineCytochrome P450 1A1enzyme
AzelastineCytochrome P450 3A5enzyme
AzelastineCytochrome P450 2C9enzyme
AzelastineCytochrome P450 2C8enzyme
AzelastineP-glycoprotein 1transporter
AzelastineCytochrome P450 2A6enzyme
AzelastineCytochrome P450 2E1enzyme
AzelastineHistamine H2 receptortarget
AzelastinePhospholipase A2target
AzelastineLeukotriene C4 synthasetarget
AzelastineCytochrome P450 2B6enzyme
PromethazineDopamine D2 receptortarget
PromethazineHistamine H1 receptortarget
PromethazineMuscarinic acetylcholine receptor M4target
PromethazineMuscarinic acetylcholine receptor M1target
PromethazineMuscarinic acetylcholine receptor M5target
PromethazineMuscarinic acetylcholine receptor M2target
PromethazineMuscarinic acetylcholine receptor M3target
PromethazineCytochrome P450 2D6enzyme
PromethazineCytochrome P450 2B6enzyme
PromethazineP-glycoprotein 1transporter
PromethazineCytochrome P450 2C9enzyme
PromethazineHistamine H2 receptortarget
PromethazineAlpha adrenergic receptortarget
PromethazineP2 Purinoceptorstarget
PromethazineVoltage-gated sodium channel alpha subunittarget
PromethazineVoltage-gated Potassium Channelstarget
PromethazineCanalicular multispecific organic anion transporter 2transporter
PromethazineMultidrug resistance-associated protein 4transporter
PromethazineSerum albumincarrier
MequitazineHistamine H1 receptortarget
MequitazineCytochrome P450 2D6enzyme
MequitazineCytochrome P450 3A4enzyme
DiphenhydramineHistamine H1 receptortarget
DiphenhydramineCytochrome P450 2D6enzyme
DiphenhydramineCytochrome P450 2C9enzyme
DiphenhydramineCytochrome P450 2C19enzyme
DiphenhydramineSolute carrier family 22 member 2transporter
DiphenhydramineSolute carrier family 22 member 5transporter
DiphenhydramineProstaglandin G/H synthase 1enzyme
DiphenhydramineMuscarinic acetylcholine receptor M2target
ChlorpheniramineHistamine H1 receptortarget
ChlorpheniramineCytochrome P450 3A4enzyme
ChlorpheniramineCytochrome P450 2D6enzyme
ChlorpheniramineSodium-dependent serotonin transportertarget
ChlorpheniramineSodium-dependent noradrenaline transportertarget
ChlorpheniramineSodium-dependent dopamine transportertarget
ChlorpheniramineCytochrome P450 3A5enzyme
ChlorpheniramineCytochrome P450 3A7enzyme
ChlorpheniramineSolute carrier family 22 member 2transporter
ChlorpheniramineSolute carrier family 22 member 1transporter
DiphenylpyralineHistamine H1 receptortarget
DiphenylpyralineSodium-dependent dopamine transportertarget
CyclizineHistamine H1 receptortarget
CyclizineEstrogen sulfotransferasetarget
CyclizineCytochrome P450 2C9enzyme
BromodiphenhydramineHistamine H1 receptortarget
BromodiphenhydramineSolute carrier family 22 member 6transporter
AlimemazineHistamine H1 receptortarget
PhenindamineHistamine H1 receptortarget
LevocetirizineHistamine H1 receptortarget
LevocetirizineSolute carrier family 22 member 11transporter
LevocetirizineCytochrome P450 3A4enzyme
LevocetirizineSerum albumincarrier
AntazolineHistamine H1 receptortarget
ChloropyramineHistamine H1 receptortarget
IsothipendylHistamine H1 receptortarget
ChlorcyclizineHistamine H1 receptortarget
AcrivastineHistamine H1 receptortarget
ThonzylamineHistamine H1 receptortarget
ThonzylamineMuscarinic acetylcholine receptor M1target
ThonzylamineMuscarinic acetylcholine receptor M2target
ThonzylamineMuscarinic acetylcholine receptor M3target
ThonzylamineMuscarinic acetylcholine receptor M4target
ThonzylamineMuscarinic acetylcholine receptor M5target
BilastineHistamine H1 receptortarget
BilastineATP-binding cassette sub-family B member 5transporter
BilastineSolute carrier organic anion transporter family member 1A2transporter
BilastineSolute carrier organic anion transporter family member 2B1transporter
RupatadineCytochrome P450 3A4enzyme
RupatadineCytochrome P450 2C9enzyme
RupatadineCytochrome P450 2C19enzyme
RupatadineCytochrome P450 2D6enzyme
RupatadinePlatelet-activating factor receptortarget
RupatadineHistamine H1 receptortarget
EbastineCytochrome P450 3A4enzyme
EbastineCytochrome P450 3A Subfamilyenzyme
MizolastineCytochrome P450 2D6enzyme
DexchlorpheniramineCytochrome P450 2D6enzyme
TripelennamineHistamine H1 receptortarget
TripelennamineCytochrome P450 2D6enzyme
PheniramineHistamine H1 receptortarget
PheniramineNuclear receptor subfamily 1 group I member 3target
PheniramineHistamine H4 receptortarget
MepyramineCytochrome P450 2D6enzyme
MepyramineHistamine H1 receptortarget
MepyramineSolute carrier family 22 member 4transporter
MepyramineSolute carrier family 22 member 5transporter
DimetindeneMuscarinic acetylcholine receptor M2target
DimetindeneHistamine H1 receptortarget